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Biological Activity for AZ 13824374
AZ 13824374 is a potent and selective inhibitor of ATPase family AAA domain-containing protein 2 (ATAD2) bromodomain (pIC50 values are 6.2 and 8.2 in NanoBRET assay and FRET assay, respectively). It is >100-fold selective over a range of epigenetic targets from ROMOscan panel (DiscoveRx Corp.). AZ 13824374 shows cellular target engagement (cellular inhibition pIC50 = 6.9) and antiproliferative activity in a range of breast cancer cell lines.
Sold with the permission of AstraZeneca UK Ltd.
Technical Data for AZ 13824374
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for AZ 13824374
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for AZ 13824374
The following data is based on the product molecular weight 562.69. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.78 mL||8.89 mL||17.77 mL|
|5 mM||0.36 mL||1.78 mL||3.55 mL|
|10 mM||0.18 mL||0.89 mL||1.78 mL|
|50 mM||0.04 mL||0.18 mL||0.36 mL|
References for AZ 13824374
References are publications that support the biological activity of the product.
Winter-Holt et al (2022) Discovery of a potent and selective ATAD2 bromodomain inhibitor with antiproliferative activity in breast cancer models. J.Med.Chem. 65 3306 PMID: 35133824
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Keywords: AZ 13824374, AZ 13824374 supplier, AZ13824374, potent, selective, inhibitors, inhibits, ATAD2, bromodomain, antiproliferative, AAA, domain-containing, protein, 2, Bromodomains, 7757, Tocris Bioscience
Citations for AZ 13824374
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Epigenetics in Cancer Poster
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Rheumatoid Arthritis Poster
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.